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Evaluation of Enzyme Inhibitors in Drug Discovery

Evaluation of Enzyme Inhibitors in Drug Discovery Author Robert A. Copeland
ISBN-10 9781118540282
Release 2013-01-31
Pages 572
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Offers essential guidance for discovering and optimizing novel drug therapies Using detailed examples, Evaluation of Enzyme Inhibitors in Drug Discovery equips researchers with the tools needed to apply the science of enzymology and biochemistry to the discovery, optimization, and preclinical development of drugs that work by inhibiting specific enzyme targets. Readers will applaud this book for its clear and practical presentations, including its expert advice on best practices to follow and pitfalls to avoid. This Second Edition brings the book thoroughly up to date with the latest research findings and practices. Updates explore additional forms of enzyme inhibition and special treatments for enzymes that act on macromolecular substrates. Readers will also find new discussions detailing the development and application of the concept of drug-target residence time. Evaluation of Enzyme Inhibitors in Drug Discovery begins by explaining why enzymes are such important drug targets and then examines enzyme reaction mechanisms. The book covers: Reversible modes of inhibitor interactions with enzymes Assay considerations for compound library screening Lead optimization and structure-activity relationships for reversible inhibitors Slow binding and tight binding inhibitors Drug-target residence time Irreversible enzyme inactivators The book ends with a new chapter exploring the application of quantitative biochemical principles to the pharmacologic evaluation of drug candidates during lead optimization and preclinical development. The Second Edition of Evaluation of Enzyme Inhibitors in Drug Discovery continues to offer a treatment of enzymology applied to drug discovery that is quantitative and mathematically rigorous. At the same time, the clear and simple presentations demystify the complex science of enzymology, making the book accessible to many fields— from pharmacology to medicinal chemistry to biophysics to clinical medicine.



Comprehensive Medicinal Chemistry III

Comprehensive Medicinal Chemistry III Author
ISBN-10 9780128032015
Release 2017-06-03
Pages 4536
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Comprehensive Medicinal Chemistry III provides a contemporary and forward-looking critical analysis and summary of recent developments, emerging trends, and recently identified new areas where medicinal chemistry is having an impact. The discipline of medicinal chemistry continues to evolve as it adapts to new opportunities and strives to solve new challenges. These include drug targeting, biomolecular therapeutics, development of chemical biology tools, data collection and analysis, in silico models as predictors for biological properties, identification and validation of new targets, approaches to quantify target engagement, new methods for synthesis of drug candidates such as green chemistry, development of novel scaffolds for drug discovery, and the role of regulatory agencies in drug discovery. Reviews the strategies, technologies, principles, and applications of modern medicinal chemistry Provides a global and current perspective of today's drug discovery process and discusses the major therapeutic classes and targets Includes a unique collection of case studies and personal assays reviewing the discovery and development of key drugs



Enzyme Kinetics Catalysis and Control

Enzyme Kinetics  Catalysis and Control Author Daniel L. Purich
ISBN-10 9780123809254
Release 2010-06-16
Pages 920
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Far more than a comprehensive treatise on initial-rate and fast-reaction kinetics, this one-of-a-kind desk reference places enzyme science in the fuller context of the organic, inorganic, and physical chemical processes occurring within enzyme active sites. Drawing on 2600 references, Enzyme Kinetics: Catalysis & Control develops all the kinetic tools needed to define enzyme catalysis, spanning the entire spectrum (from the basics of chemical kinetics and practical advice on rate measurement, to the very latest work on single-molecule kinetics and mechanoenzyme force generation), while also focusing on the persuasive power of kinetic isotope effects, the design of high-potency drugs, and the behavior of regulatory enzymes. Historical analysis of kinetic principles including advanced enzyme science Provides both theoretical and practical measurements tools Coverage of single molecular kinetics Examination of force generation mechanisms Discussion of organic and inorganic enzyme reactions



Drug Discovery

Drug Discovery Author Jie Jack Li
ISBN-10 9781118354469
Release 2013-04-03
Pages 570
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Sets forth the history, state of the science, and future directions of drug discovery Edited by Jie Jack Li and Nobel laureate E. J. Corey, two leading pioneers in drug discovery and medicinal chemistry, this book synthesizes great moments in history, the current state of the science, and future directions of drug discovery into one expertly written and organized work. Exploring all major therapeutic areas, the book introduces readers to all facets and phases of drug discovery, including target selection, biological testing, drug metabolism, and computer-assisted drug design. Drug Discovery features chapters written by an international team of pharmaceutical and medicinal chemists. Contributions are based on a thorough review of the current literature as well as the authors' firsthand laboratory experience in drug discovery. The book begins with the history of drug discovery, describing groundbreaking moments in the field. Next, it covers such topics as: Target identification and validation Drug metabolism and pharmacokinetics Central nervous system drugs In vitro and in vivo assays Cardiovascular drugs Cancer drugs Each chapter features a case study, helping readers understand how science is put into practice throughout all phases of drug discovery. References at the end of each chapter serve as a gateway to groundbreaking original research studies and reviews in the field. Drug Discovery is ideal for newcomers to medicinal chemistry and drug discovery, providing a comprehensive overview of the field. Veterans in the field will also benefit from the perspectives of leading international experts in all aspects of drug discovery.



Thermodynamics and Kinetics of Drug Binding

Thermodynamics and Kinetics of Drug Binding Author György Keserü
ISBN-10 9783527673056
Release 2015-03-09
Pages 360
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This practical reference for medicinal and pharmaceutical chemists combines the theoretical background with modern methods as well as applications from recent lead finding and optimization projects. Divided into two parts on the thermodynamics and kinetics of drug-receptor interaction, the text provides the conceptual and methodological basis for characterizing binding mechanisms for drugs and other bioactive molecules. It covers all currently used methods, from experimental approaches, such as ITC or SPR, right up to the latest computational methods. Case studies of real-life lead or drug development projects are also included so readers can apply the methods learned to their own projects. Finally, the benefits of a thorough binding mode analysis for any drug development project are summarized in an outlook chapter written by the editors.



ADMET for Medicinal Chemists

ADMET for Medicinal Chemists Author Katya Tsaioun
ISBN-10 0470922818
Release 2011-02-15
Pages 512
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This book guides medicinal chemists in how to implement early ADMET testing in their workflow in order to improve both the speed and efficiency of their efforts. Although many pharmaceutical companies have dedicated groups directly interfacing with drug discovery, the scientific principles and strategies are practiced in a variety of different ways. This book answers the need to regularize the drug discovery interface; it defines and reviews the field of ADME for medicinal chemists. In addition, the scientific principles and the tools utilized by ADME scientists in a discovery setting, as applied to medicinal chemistry and structure modification to improve drug-like properties of drug candidates, are examined.



Case Studies in Modern Drug Discovery and Development

Case Studies in Modern Drug Discovery and Development Author Xianhai Huang
ISBN-10 9780470601815
Release 2012-05-29
Pages 472
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Learn why some drug discovery and development efforts succeed . . . and others fail Written by international experts in drug discovery and development, this book sets forth carefully researched and analyzed case studies of both successful and failed drug discovery and development efforts, enabling medicinal chemists and pharmaceutical scientists to learn from actual examples. Each case study focuses on a particular drug and therapeutic target, guiding readers through the drug discovery and development process, including drug design rationale, structure-activity relationships, pharmacology, drug metabolism, biology, and clinical studies. Case Studies in Modern Drug Discovery and Development begins with an introductory chapter that puts into perspective the underlying issues facing the pharmaceutical industry and provides insight into future research opportunities. Next, there are fourteen detailed case studies, examining: All phases of drug discovery and development from initial idea to commercialization Some of today's most important and life-saving medications Drugs designed for different therapeutic areas such as cardiovascular disease, infection, inflammation, cancer, metabolic syndrome, and allergies Examples of prodrugs and inhaled drugs Reasons why certain drugs failed to advance to market despite major research investments Each chapter ends with a list of references leading to the primary literature. There are also plenty of tables and illustrations to help readers fully understand key concepts, processes, and technologies. Improving the success rate of the drug discovery and development process is paramount to the pharmaceutical industry. With this book as their guide, readers can learn from both successful and unsuccessful efforts in order to apply tested and proven science and technologies that increase the probability of success for new drug discovery and development projects.



The Handbook of Medicinal Chemistry

The Handbook of Medicinal Chemistry Author Andrew Davis
ISBN-10 9781782621836
Release 2015-07-07
Pages 753
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Drug discovery is a constantly developing and expanding area of research. Developed to provide a comprehensive guide, the Handbook of Medicinal Chemistry covers the past, present and future of the entire drug development process. Highlighting the recent successes and failures in drug discovery, the book helps readers to understand the factors governing modern drug discovery from the initial concept through to a marketed medicine. With chapters covering a wide range of topics from drug discovery processes and optimization, development of synthetic routes, pharmaceutical properties and computational biology, the handbook aims to enable medicinal chemists to apply their academic understanding to every aspect of drug discovery. Each chapter includes expert advice to not only provide a rigorous understanding of the principles being discussed, but to provide useful hints and tips gained from within the pharmaceutical industry. This expertise, combined with project case studies, highlighting and discussing all areas of successful projects, make this an essential handbook for all those involved in pharmaceutical development. A free iPad app has been created in collaboration with the editors of the book. The Medicinal Chemistry Toolkit provides a suite of resources to support the day to day work of a medicinal chemist. Search for "Medicinal Chemistry Toolkit."



Privileged Structures in Drug Discovery

Privileged Structures in Drug Discovery Author Larry Yet
ISBN-10 9781118145661
Release 2018-03-27
Pages 560
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A comprehensive guide to privileged structures and their application in the discovery of new drugs The use of privileged structures is a viable strategy in the discovery of new medicines at the lead optimization stages of the drug discovery process. Privileged Structures in Drug Discovery offers a comprehensive text that reviews privileged structures from the point of view of medicinal chemistry and contains the synthetic routes to these structures. In this text, the author—a noted expert in the field—includes an historical perspective on the topic, presents a practical compendium to privileged structures, and offers an informed perspective on the future direction for the field. The book describes the up-to-date and state-of-the-art methods of organic synthesis that describe the use of privileged structures that are of most interest. Chapters included information on benzodiazepines, 1,4-dihydropyridines, biaryls, 4-(hetero)arylpiperidines, spiropiperidines, 2-aminopyrimidines, 2-aminothiazoles, 2-(hetero)arylindoles, tetrahydroisoquinolines, 2,2-dimethylbenzopyrans, hydroxamates, and bicyclic pyridines containing ring-junction nitrogen as privileged scaffolds in medicinal chemistry. Numerous, illustrative case studies document the current use of the privileged structures in the discovery of drugs. This important volume: Describes the drug compounds that have successfully made it to the marketplace and the chemistry associated with them Offers the experience from an author who has worked in many therapeutic areas of medicinal chemistry Details many of the recent developments in organic chemistry that prepare target molecules Includes a wealth of medicinal chemistry case studies that clearly illustrate the use of privileged structures Designed for use by industrial medicinal chemists and process chemists, academic organic and medicinal chemists, as well as chemistry students and faculty, Privileged Structures in Drug Discovery offers a current guide to organic synthesis methods to access the privileged structures of interest, and contains medicinal chemistry case studies that document their application.



Drug Discovery and Development E Book

Drug Discovery and Development   E Book Author Raymond G Hill
ISBN-10 9780702053160
Release 2012-07-20
Pages 368
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The modern pharmacopeia has enormous power to alleviate disease, and owes its existence almost entirely to the work of the pharmaceutical industry. This book provides an introduction to the way the industry goes about the discovery and development of new drugs. The first part gives a brief historical account from its origins in the mediaeval apothecaries’ trade, and discusses the changing understanding of what we mean by disease, and what therapy aims to achieve, as well as summarising case histories of the discovery and development of some important drugs. The second part focuses on the science and technology involved in the discovery process: the stages by which a promising new chemical entity is identified, from the starting point of a medical need and an idea for addressing it. A chapter on biopharmaceuticals, whose discovery and development tend to follow routes somewhat different from synthetic compounds, is included here, as well as accounts of patent issues that arise in the discovery phase, and a chapter on research management in this environment. The third section of the book deals with drug development: the work that has to be undertaken to turn the drug candidate that emerges from the discovery process into a product on the market. The definitive introduction to how a pharmaceutical company goes about its business of discovering and developing drugs. The second edition has a new editor: Professor Raymond Hill ● non-executive director of Addex Pharmaceuticals, Covagen and of Orexo AB ● Visiting Industrial Professor of Pharmacology in the University of Bristol ● Visiting Professor in the School of Medical and Health Sciences at the University of Surrey ● Visiting Professor in Physiology and Pharmacology at the University of Strathclyde ● President and Chair of the Council of the British Pharmacological Society ● member of the Nuffield Council on Bioethics and the Advisory Council on Misuse of Drugs. New to this edition: Completely rewritten chapter on The Role of Medicinal Chemistry in the Drug Discovery Process. New topic - DMPK Optimization Strategy in drug discovery. New chapter on Scaffolds: Small globular proteins as antibody substitutes. Totally updated chapters on Intellectual Property and Marketing 50 new illustrations in full colour Features Accessible, general guide to pharmaceutical research and development. Examines the interfaces between cost and social benefit, quality control and mass production, regulatory bodies, patent management, and all interdisciplinary intersections essential to effective drug development. Written by a strong team of scientists with long experience in the pharmaceutical industry. Solid overview of all the steps from lab bench to market in an easy-to-understand way which will be accessible to non-specialists. From customer reviews of the previous edition: ‘... it will have everything you need to know on this module. Deeply referenced and, thus, deeply reliable. Highly Commended in the medicine category of the BMA 2006 medical book competition Winner of the Royal Society of Medicine Library Prize for Medical Book of the Year



The Practice of Medicinal Chemistry

The Practice of Medicinal Chemistry Author C. G. Wermuth
ISBN-10 9780127444819
Release 2003
Pages 768
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Most medicinal chemists working in the pharmaceutical industry are organic synthetic chemists with little or no background in medicinal chemistry. These chemists must acquire a good knowledge of medicinal chemistry during their first years in the pharmaceutical/drug discovery industry. This book aims to be their practical handbook - a complete guide to the drug discovery process. The book reviews practical aspects of Medicinal Chemistry, emphasising the daily problems met by the medicinal chemist when dealing with lead discovery/identification methodologies, with structure-activity relationship studies aimed to scale up potency and target selectivity, and when optimising pharmacokinetic and pharmaceutical properties by means of ultimate chemical modifications. This is the second edition of The Practice of Medicinal Chemistry, the first edition being published in February 1996. The new edition is thoroughly revised, with around 30% new material, and refocussed to reflect the recent developments in genomics, proteomics, high throughput screening of compounds and drug solubilisation. An effort has been made to remove the overlap that exists in the previous edition and four new chapters have been introduced. * Written by experts in the field * The first edition of The Practice of Medicinal Chemistry, published in 1996, was nicknamed 'The Bible' by medicinal chemists. * The only available book dealing with the practical aspects of medicinal chemistry, from conception of the molecules through to the production of drugs * An essential practical handbook for the medicinal chemist, working in the pharmaceutical industry, with little or no background in medicinal chemistry-a complete guide to the drug discovery process.



Drug Selectivity

Drug Selectivity Author Norbert Handler
ISBN-10 9783527335381
Release 2018-02-05
Pages 536
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The book provides a current overview and comprehensive compilation for medicinal chemists that discusses the effects of aiming for multiple targets on the entire drug development process. The result is a broad survey of current and future strategies for drug selectivity in medicinal chemistry with theoretical but also practical aspects. Different strategies are presented and evaluated, such as various design approaches, merged multiple ligands, discovery technologies and a broad range of successful examples of unselective drugs taken from all major disease areas. With its wide-ranging view of an emerging new paradigm in drug development, this handbook is of prime importance for every medicinal and pharmaceutical chemist.



ADME Enabling Technologies in Drug Design and Development

ADME Enabling Technologies in Drug Design and Development Author Donglu Zhang
ISBN-10 9780470542781
Release 2012-04-30
Pages 591
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This book comprehensively covers the state-of-the-art and cutting-edge technologies in an integrated fashion for applications in ADME studies of small molecular drugs. Each chapter provides descriptions of the technologies, application scope and limitations, optimal conditions for intended results, protocols, case studies, and future developments. By concisely describing these technologies, the book provides a useful tool for drug metabolism scientists and as a reference for scientists in the fields of pharmacology, medicinal chemistry, pharmaceutics, toxicology, bioanalytical science in academia and industry.



Advances in Drug Discovery Techniques

Advances in Drug Discovery Techniques Author Alan L. Harvey
ISBN-10 0471975095
Release 1998-08-15
Pages 222
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A guide to techniques for the discovery and evaluation of pharamcologically active compounds for therapeutic development, this book covers rational drug design, high-throughput screening, and genetic approaches to drug discovery. The authors focus on advances in the use of combinatorial chemistry and natural products, both of which support the chemical diversity for many drug screening programmes. They examine typical screening studies and their link to robotics and informatics in detail and present an overview of current progress within anitsense therapeutics. The book explores the rapid changes in drug discovery resulting from developments in molecular biology, robotics, and informatics.



Preclinical Drug Development Second Edition

Preclinical Drug Development  Second Edition Author Mark Rogge
ISBN-10 9781420084733
Release 2016-04-19
Pages 376
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Preclinical Drug Development, Second Edition discusses the broad and complicated realm of preclinical drug development. Topics range from assessment of pharmacology and toxicology to industry trends and regulatory expectations to requirements that support clinical trials. Highlights of the Second Edition include: Pharmacokinetics Modeling and simulation Formulation and routes of administration Toxicity evaluations The assessment of drug absorption and metabolism Interspecies scaling Lead molecule selection and optimization via profiling Screening using in silico and in vitro toxicity evaluations The book also includes case studies on preclinical pharmacokinetic-pharmacodynamic modeling and simulation in drug development, a review of ICH preclinical guidelines, and experimental methods used to study membrane drug transport and metabolism. This guide is a fundamental resource for medicinal chemists, biologists, and other specialists in the drug development sciences.



Drug Discovery and Evaluation Methods in Clinical Pharmacology

Drug Discovery and Evaluation  Methods in Clinical Pharmacology Author Hans Georg Vogel
ISBN-10 9783540898900
Release 2010-12-15
Pages 564
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These volumes are a landmark in the continuously changing world of drugs an easy-to-use, method-oriented overview on all aspects of clinical pharmacology Essential reading for pharmacologists, physicians, medicinal chemists and pharmacists at research institutes and in industry of use for governmental institutions and committees working on official guidelines for drug evaluation worldwide Drug Discovery and Evaluation has become a more and more difficult, expensive and time-consuming process. the effect of a new compound has to be detected by in vitro and in vivo methods of pharmacology. the a



Successful Drug Discovery

Successful Drug Discovery Author János Fischer
ISBN-10 9783527808663
Release 2018-04-09
Pages 364
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With its focus on drugs so recently introduced that they have yet to be found in any other textbooks or general references, the information and insight found here makes this a genuinely unique handbook and reference. Following the successful approach of the previous volumes in the series, inventors and primary developers of successful drugs from both industry and academia tell the story of the drug's discovery and describe the sometimes twisted route from the first drug candidate molecule to the final marketed drug. The 11 case studies selected describe recent drugs ranging across many therapeutic fields and provide a representative cross-section of present-day drug developments. Backed by plenty of data and chemical information, the insight and experience of today?s top drug creators makes this one of the most useful training manuals that a junior medicinal chemist may hope to find. The International Union of Pure and Applied Chemistry has endorsed and sponsored this project because of its high educational merit.